Patents Examined by D. Dinner
-
Patent number: 4771054Abstract: Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.Type: GrantFiled: August 15, 1986Date of Patent: September 13, 1988Assignee: Warner-Lambert CompanyInventors: John M. Domagala, Thomas F. Mich, Jeffrey B. Nichols
-
Patent number: 4765974Abstract: A clonidine preparation for percutaneous administration comprising a support having provided thereon an active ingredient-containing layer is disclosed. The active ingredient-containing layer contains an acrylic polymer having a glass transition temperature of from -70.degree. C. to -10.degree. C. and pressure-sensitive adhesion at room temperature as a base, at least one of clonidine and clonidine hydrochloride as an active ingredient, and a decomposition inhibitor. The active ingredient can be stably maintained within the preparation without being decomposed, and, therefore, can be effectively released over a prolonged period of time.Type: GrantFiled: May 13, 1987Date of Patent: August 23, 1988Assignee: Nitto Electric Industrial Co., Ltd.Inventors: Shoichi Tokuda, Yuusuke Ito, Saburo Otsuka, Takashi Kinoshita
-
Patent number: 4758670Abstract: Fluoroazolylpropane derivatives of the formula I ##STR1## are described, in which Az is imidazolyl or triazolyl, R.sup.1 is hydrogen, alkyl or aralkyl which is unsubstituted or substituted by halogen, alkyl, alkoxy, halogenoalkyl, nitro, cyano, carboxyl or alkoxycarbonyl, R.sup.2 is C.sub.1 -C.sub.10 -alkyl which is unsubstituted or substituted by alkoxy, aralkoxy or phenyl, it being possible for the aromatic nuclei of aralkoxy and phenyl in turn to be unsubstituted or substituted by halogen, alkyl, alkoxy, halogenoalkyl, cyano, carboxyl or alkoxycarbonyl, R.sup.3 is hydrogen, alkyl, alkylcarbonyl or aralkyl which is unsubstituted or substituted by halogen, alkoxy, alkyl, halogenoalkyl, cyano, carboxyl or alkoxycarbonyl, R.sup.5 is an unsubstituted or monosubstituted or polysubstituted radical selected from the series comprising C.sub.1 -C.sub.8 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.Type: GrantFiled: January 4, 1984Date of Patent: July 19, 1988Assignee: Ciba-Geigy CorporationInventors: Urs Muller, Hermann Rempfler, Hans Tobler
-
Patent number: 4749405Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group, R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof; are outstandingly effective plant growth regulants and as fungicides.Type: GrantFiled: August 8, 1986Date of Patent: June 7, 1988Assignee: Bayer AktiengesellschaftInventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
-
Patent number: 4743293Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;X is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group, R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof;are outstandingly effective plant growth regulants and as fungicides.Type: GrantFiled: July 30, 1986Date of Patent: May 10, 1988Assignee: Bayer AktiengesellschaftInventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
-
Patent number: 4737497Abstract: Disclosed are novel bis-dioxopiperazine derivatives, process for their preparation, antitumor agents comprising them and compositions containing them.The bis-dioxopiperazine derivatives are represented by the following general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms; R.sub.2 represents a hydrogen atom or a group of ##STR2## R.sub.3 and R.sub.4, which are respectively independent and are the same or different, represent respectively a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms or a heterocyclic radical selected from the group consisting of substituted or unsubstituted piperidino, substituted or unsubstituted piperazino, substituted or unsubstituted morpholino and substituted or unsubstituted thiomorpholino, or R.sub.3 and R.sub.Type: GrantFiled: April 4, 1984Date of Patent: April 12, 1988Assignee: Zenyaki Kogyo Kabushiki KaishaInventor: Yun-feng Ren
-
Patent number: 4703128Abstract: The feature of the present invention is a process for preparing compounds represented by general formula (Ia) described below: ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, R.sub.1, R.sub.2, R.sub.3 and R.sub.7 are as defined in formula (I) and R.sub.10 represents a lower alkyl group, or acid salts thereof, which process is characterized by using the guanidylfungins (II) as raw materials, reacting these guanidylfungins with alcohols (III) in the presence of an acid catalyst, and then hydrolyzing the malonic acid monoester (IV).Type: GrantFiled: July 18, 1986Date of Patent: October 27, 1987Assignee: Takahara Shuzo Co., Ltd.Inventors: Teruhiko Beppu, Kazutoh Takesako, Teruya Nakamura, Akira Obayashi
-
Patent number: 4699777Abstract: A topical albuterol composition having superior transdermal flux containing various amounts of albuterol, 1-dodecyl-azacycloheptan-2-one and urea in a non-aqueous environment. The enhancement observed in albuterol skin penetration indicates that a therapeutically effective amount of albuterol can be delivered through skin using these formulations. The compositions can be administered topically as a cream, lotion or via a transdermal device.Type: GrantFiled: August 21, 1985Date of Patent: October 13, 1987Assignee: Schering CorporationInventors: Michael A. Zupon, Joel A. Sequeira
-
Patent number: 4696945Abstract: The invention relates to parasiticidally and insecticidally highly active compounds of formula I ##STR1## wherein R.sub.1 is hydrogen or a protecting group;R.sub.2 is methyl, ethyl, isopropyl or sec-butyl; andR is a radical R.sub.3 which is bound through oxygen or sulfur and is selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 haloalkyl, C.sub.1 -C.sub.10 hydroxyalkyl, C.sub.1 -C.sub.10 mercaptoalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.3 -C.sub.10 alkoxyalkoxyalkyl, hydroxy- or mercapto-substituted C.sub.3 -C.sub.10 alkoxyalkyl, C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalky, hdroxy- or mercapto-substituted C.sub.4 -C.sub.15 alkoxyalkoxyalkoxyalkyl, C.sub.2 -C.sub.10 -alkenyl, C.sub.2 -C.sub.10 haloalkenyl, C.sub.2 -C.sub.10 alkynyl, C.sub.2 -C.sub.10 haloalkynyl, phenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.Type: GrantFiled: July 14, 1986Date of Patent: September 29, 1987Assignee: Ciba-Geigy CorporationInventors: Bruno Frei, Anthony C. O'Sullivan
-
Patent number: 4684392Abstract: New substituted .beta.-triazolyl oximes, processes for their manufacture, agents for regulating plant growth containing these compounds, and a process for regulating plant growth with these compounds.Type: GrantFiled: January 9, 1985Date of Patent: August 4, 1987Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Hubert Sauter, Bernd Zeeh, Gerd Heilen, Johann Jung
-
Patent number: 4670454Abstract: Azolylmethylcycloalkanes of the formula I ##STR1## where A and B are identical or different and are each hydrogen, unsubstituted or halogen-substituted alkyl of 1 to 4 carbon atoms, naphthyl, hetaryl, biphenyl or phenyl, where the phenyl radical can be substituted by halogen, nitro, alkyl, alkoxy or haloalkyl, each of 1 to 4 carbon atoms, phenoxy or phenylsulfenyl, D and E are identical or different and are each hydrogen or halogen, Z is CH or N, m can be 1, 2, 3 or 4 and n can be 0, 1 or 2, their addition salts with acids and their metal complexes, and the preparation of these compounds, are described. The compounds are useful for treating disorders and for crop, wood and material protection.Type: GrantFiled: February 29, 1984Date of Patent: June 2, 1987Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Norbert Meyer, Ernst-Heinrich Pommer, Eberhard Ammermann, Friedrich-Wilhelm Kohlmann, Walter Wesenberg, Wolfgang Heberle
-
Patent number: 4666699Abstract: A stain-fixative composition, for use in the microscopic identification of enteric protozoa and other parasites in fecal specimens, contains Ponceau S Stain, Chlorazol Fast Pink BK Stain, Trypan Blue Stain, dimethyl sulfoxide and a fixative component. The fixative component may be either a polyvinyl alcohol fixative or may be a mixture of isopropanol, acetic acid, liquified phenol, distilled water and optional glutaraldehyde. The stain-fixative composition is simple to prepare, has a long shelf life at ambient conditions, is easy to use and is suitable for preparing formalin or tap water concentrates, wet mount slides, or permanent smears prepared with gelatin-glycerol or resinous mounting media. In addition, the stain-fixative composition is free from the toxic mercury compounds often found in prior art staining reagents. The stain-fixative composition gives superior fixation and resolution, yet its use requires a minimum of time and attention in the laboratory.Type: GrantFiled: March 4, 1985Date of Patent: May 19, 1987Assignee: Allegheny-Singer Research InstituteInventor: Malcolm Slifkin
-
Patent number: 4661507Abstract: Compounds of the general formula: ##STR1## wherein R is naphthyl, biphenylyl, phenyl or substituted phenyl; n is 0, 1 or 2; and R.sup.1 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkanoyl, or C.sub.1-2 alkyl substituted by C.sub.2-4 alkenyl with the provisos that when R.sup.1 is H or C.sub.2-4 alkanoyl, n is 0; and when n is 2, R.sup.1 is C.sub.1-3 alkyl; and their pharmaceutically acceptable salts are antifungal agents useful in combatting fungal infections in animals, including humans.Type: GrantFiled: August 28, 1984Date of Patent: April 28, 1987Assignee: Pfizer Inc.Inventors: Geoffrey E. Gymer, Kenneth Richardson
-
Patent number: 4658025Type: GrantFiled: December 21, 1984Date of Patent: April 14, 1987Assignee: Bayer AktiengesellschaftInventor: Fritz Maurer
-
Patent number: 4647302Abstract: 1-Vinyltriazole compounds of the formula ##STR1## wherein R.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl;R.sup.2 is alkyl;R.sup.3 is alkyl, cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkenyl, aryl or substituted aryl; orR.sup.2 and R.sup.3, together with the carbon to which they are bonded, represent cycloalkenyl, substituted cycloalkenyl, cycloalkyl or substituted cycloalkyl;X is the group ##STR2## or, alternatively, X may represent a keto group provided that when X is a keto group R.sup.1 is alkyl, substituted alkyl, cycloalkyl, or substituted cycloalkyl;R.sup.4 is hydrogen, alkyl, aralkyl, substituted aralkyl, acyl, carbamoyl or substituted carbamoyl;R.sup.5 is hydrogen, alkyl, aralkyl or substituted aralkyl;and acid addition salts and metal salt complexes thereof; are outstandingly effective plant growth regulants and as fungicides.Type: GrantFiled: June 12, 1984Date of Patent: March 3, 1987Assignee: Bayer AktiengesellschaftInventors: Wolf Reiser, Wilfried Draber, Karl H. Buchel, Klaus Lurssen, Paul-Ernst Frohberger, Volker Paul
-
Patent number: 4639524Abstract: Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoracetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.Type: GrantFiled: July 9, 1984Date of Patent: January 27, 1987Assignee: G. D. Searle & Co.Inventors: Bipinchandra N. Desai, Robert J. Chorvat, Kurt J. Rorig
-
Patent number: 4638067Abstract: Novel naphthyridine-, quinoline- and benzoxazine-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.Type: GrantFiled: August 12, 1985Date of Patent: January 20, 1987Assignee: Warner-Lambert Co.Inventors: Townley P. Culbertson, John M. Domagala, Thomas F. Mich, Jeffrey B. Nichols
-
Patent number: 4636247Abstract: Triazoles and imidazoles of the formula (I): ##STR1## and stereoisomers thereof, wherein W is CH or N; Q is optionally substituted aryl (especially optionally substituted phenyl), optionally substituted aralkyl, or alkyl; R.sup.1 is H, alkyl, cycloalkyl, alkenyl, alkynyl, acyl, optionally substituted aralkyl, optionally substituted phenyl, or is an alkyl or aralkyl group substituted with an ether, hydroxyl, carboxylic ester, or ketone group; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are H, alkyl, cycloalkyl, optionally substituted aralkyl, or optionally substituted phenyl; and acid salts and metal complexes thereof. These compounds are useful as plant growth regulators and fungicides. Other values for R.sup.1 include C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkoxyalkyl and phenyl or benzyl substituted by benzyl.Type: GrantFiled: February 8, 1984Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Timothy Lewis, Michael B. Gravestock
-
Patent number: 4634783Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.Type: GrantFiled: January 23, 1984Date of Patent: January 6, 1987Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Ryoji Matsui, Shin-ichi Watanabe, Kimio Sudo, Toshiyuki Okutome, Masateru Kurumi, Yojiro Sakurai, Takuo Aoyama
-
Patent number: 4597903Abstract: A process for the direct preparation of N,N-disubstituted derivatives of 4,13-diaza-18-crown-6 in which the substituents on both nitrogen atoms are identical and derive originally from an amine, by reacting a 1,8-diiodo-3,6-dioxooctane or derivatives thereof in which the substituents are located on positions 1, 2, 4, 5, 7 or 8 or combinations thereof, with a molar equivalent of a primary amine in the presence of a base and solvent.Type: GrantFiled: August 21, 1984Date of Patent: July 1, 1986Assignee: University of MarylandInventors: George W. Gokel, Vincent J. Gatto